Structure of the neurotensin receptor 1 in complex with β-arrestin 1

W Huang, M Masureel, Q Qu, J Janetzko, A Inoue… - Nature, 2020 - nature.com
Arrestin proteins bind to active, phosphorylated G-protein-coupled receptors (GPCRs),
thereby preventing G-protein coupling, triggering receptor internalization and affecting …

[HTML][HTML] Membrane phosphoinositides regulate GPCR-β-arrestin complex assembly and dynamics

J Janetzko, R Kise, B Barsi-Rhyne, DH Siepe… - Cell, 2022 - cell.com
Binding of arrestin to phosphorylated G protein-coupled receptors (GPCRs) is crucial for
modulating signaling. Once internalized, some GPCRs remain complexed with β-arrestins …

Targeting GRK2 and GRK5 for treating chronic degenerative diseases: Advances and future perspectives

Y Zhang, J Zhang, J Wang, H Chen, L Ouyang… - European Journal of …, 2022 - Elsevier
The development of small-molecule inhibitors targeting G protein-coupled receptor kinase 2
(GRK2) and G protein-coupled receptor kinase 5 (GRK5) for the treatment of chronic …

Targeting G protein–coupled receptor kinases to G protein–coupled receptors

SM Sulon, JL Benovic - Current opinion in endocrine and metabolic …, 2021 - Elsevier
G protein–coupled receptors (GPCRs) interact with three protein families after agonist
binding: heterotrimeric G proteins, G protein–coupled receptor kinases (GRKs), and …

GRK5 is a regulator of fibroblast activation and cardiac fibrosis

A Eguchi, R Coleman, K Gresham… - Proceedings of the …, 2021 - National Acad Sciences
Pathological remodeling of the heart is a hallmark of chronic heart failure (HF) and these
structural changes further perpetuate the disease. Cardiac fibroblasts are the critical cell …

Negative allosteric modulation of the glucagon receptor by RAMP2

KK Kumar, ES O'Brien, CH Habrian, NR Latorraca… - Cell, 2023 - cell.com
Receptor activity-modifying proteins (RAMPs) modulate the activity of many Family B
GPCRs. We show that RAMP2 directly interacts with the glucagon receptor (GCGR), a …

Mapping interactions of calmodulin and neuronal NO synthase by crosslinking and mass spectrometry

D Felker, K Lee, TH Pospiech, Y Morishima… - Journal of Biological …, 2024 - ASBMB
Neuronal nitric oxide synthase (nNOS) is a homodimeric cytochrome P450-like enzyme that
catalyzes the conversion of L-arginine to nitric oxide in the presence of NADPH and …

Protein tyrosine phosphatase 1B inhibitors from the fungus Malbranchea albolutea

M Díaz-Rojas, H Raja, M González-Andrade… - Phytochemistry, 2021 - Elsevier
From solid rice-based cultures of Malbranchea albolutea, three undescribed ardeemins and
sartoryglabrins analogs were discovered and named alboluteins AC. 1H-Indole-3 …

Structure of a GRK5-calmodulin complex reveals molecular mechanism of GRK activation and substrate targeting

KE Komolov, SM Sulon, A Bhardwaj, SC van Keulen… - Molecular cell, 2021 - cell.com
The phosphorylation of G protein-coupled receptors (GPCRs) by GPCR kinases (GRKs)
facilitates arrestin binding and receptor desensitization. Although this process can be …

Antagonistic roles of GRK2 and GRK5 in cardiac aldosterone signaling reveal GRK5-mediated cardioprotection via mineralocorticoid receptor inhibition

J Maning, KA McCrink, CM Pollard… - International Journal of …, 2020 - mdpi.com
Aldosterone (Aldo), when overproduced, is a cardiotoxic hormone underlying heart failure
and hypertension. Aldo exerts damaging effects via the mineralocorticoid receptor (MR) but …